Adinazolam is now an accepted generic name for 8-chloro-1-[(dimethylamino)methyl]-6-phenyl-4H-s-triazolo[4,3-a][1,4]benzo diazepine, and is described and claimed among other compounds in U.S. Pat. No. 4,250,094.
Laboratory studies of chemical compounds as possible antipsychotic drugs have taken the form of observation of effects caused by administration of test compounds in vivo in the .sup.3 H-Spiroperidol Binding Test which is a standard laboratory animal test for determining whether or not the compound might have activity in combatting psychoses, including schizophrenia in humans in later tests. Compounds defined hereinbelow have shown promising activities in this test.
In humans, studies of the use of candidate drug compounds as antipsychotic drugs have focused on the ability of those drug candidate compounds to control the positive symptoms of schizophrenia such as delusions, hallucinations, positive thought disorder and bizzare behavior. However, it is widely understood that treated schizophrenics remain a problem to themselves and society because of negative symptoms including flattened affect, poverty of expression (alogia), lack of initiative (avolition), anhedonia, attentional impairment and hyposocialization. See "Negative v Positive Schizophrenia" by N. C. Andreason et al. in Arch. Gen. Psychiatry, 39, pp. 789-794 (1982).
Adinazolam and some other 1-amino-triazolo-benzodiazepines have undergone preliminary testing in their in vivo .sup.3 H-Spiroperidol binding system test in animals, which test is highly selective for antipsychotic active drug compounds. Test results with adinazolam were weak but suggested antipsychotic-like activity. A variety of other compounds of this invention also showed activity in this test.
Antipsychotic activity has been found for the well known benzodiazepine, diazepam. See "Acute High Dose Parenteral Haloperidol Treatment of Psychosis" by Y. Lerner et al. in American J. Psychiatry, 136, pp. 1061-1064 (1979), where the authors report that diazepam was at least as effective as haloperidol over 24 hours of treatment for acute psychosis, but it was also reported that marked sedation effects hampered further consideration of diazepam as an antipsychotic drug of choice.
Those in the art continue to search for antipsychotic drug compounds which will be effective for treating and alleviating the conditions caused by psychoses, including schizophrenia, and at the same time not cause any substantial sedation or hypnotic effects in the patients being treated.